Ring Oxygen In The Bicyclo Ring System Patents (Class 514/302)
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Publication number: 20130030014Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 11, 2012Publication date: January 31, 2013Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Publication number: 20130029949Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: July 20, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
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Publication number: 20130029995Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
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Publication number: 20130023557Abstract: The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.Type: ApplicationFiled: June 25, 2012Publication date: January 24, 2013Applicant: SANOFIInventors: Dieter KADEREIT, Matthias SCHAEFER, Stephanie HACHTEL, Thomas HUEBSCHLE, Katrin HISS
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Publication number: 20130023525Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: April 24, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Publication number: 20130023558Abstract: Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.Type: ApplicationFiled: June 25, 2012Publication date: January 24, 2013Applicant: SANOFIInventors: Dieter KADEREIT, Matthias SCHAEFER, Stephanie HACHTEL, Thomas HUEBSCHLE, Katrin HISS
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Patent number: 8357682Abstract: The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: GrantFiled: May 5, 2008Date of Patent: January 22, 2013Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Theodros Asberom, Xianhai Huang, Xiaohong Zhu, Mark D. McBriar, Dmitri A. Pissarnitski, Zhiqiang Zhao, Ruo Xu, Hongmei Li, Anandan Palani, Johannes H. Voigt, Robert D. Mazzola, Jr., John Clader, Hubert Josien, Jun Qin
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130018030Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: January 20, 2012Publication date: January 17, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE
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Patent number: 8354426Abstract: Disclosed is 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate, which has strong antibacterial activity. The compound is highly safe and useful as an original drug for pharmaceutical preparations. Also disclosed is a method which is useful for producing 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate.Type: GrantFiled: November 25, 2008Date of Patent: January 15, 2013Assignees: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Taro Kiyoto, Masahiro Takebayashi, Yasutaka Baba, Muneo Syoji, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
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Publication number: 20130012530Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.Type: ApplicationFiled: July 6, 2012Publication date: January 10, 2013Applicant: H. Lundbeck A/SInventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
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Patent number: 8349829Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH?CH-E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.Type: GrantFiled: June 2, 2009Date of Patent: January 8, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8349864Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient or carrier and a compound Formula I: or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: March 19, 2009Date of Patent: January 8, 2013Assignee: New Mexico Technical Research FoundationInventors: Alexander Kornienko, Igov V. Magedov, Snezna Rogelj
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Publication number: 20130005655Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Applicant: Somaxon Pharmaceuticals, Inc.Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Publication number: 20120329827Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection and AIDS.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Applicant: Ambrilia Biopharma, Inc.Inventors: Brent Richard Stranix, Guy Milot, Jean-Emmanuel Bouchard
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Publication number: 20120329772Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: ApplicationFiled: July 9, 2012Publication date: December 27, 2012Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li
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Publication number: 20120322784Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
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Publication number: 20120316195Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 16, 2010Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
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Publication number: 20120316196Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.Type: ApplicationFiled: August 23, 2012Publication date: December 13, 2012Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
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Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
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Patent number: 8324239Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: April 19, 2011Date of Patent: December 4, 2012Assignee: Novartis AGInventors: David Barnes, Rajiv Chopra, Scott Louis Cohen, Jiping Fu, Mitsunori Kato, Peichao Lu, Mohindra Seepersaud, Wei Zhang
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Publication number: 20120302576Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Publication number: 20120289542Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome.Type: ApplicationFiled: January 17, 2012Publication date: November 15, 2012Inventors: Benson M. Fong, Glenn V. Cornett
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Publication number: 20120289497Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: ApplicationFiled: January 17, 2011Publication date: November 15, 2012Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20120283260Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: July 24, 2012Publication date: November 8, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120270864Abstract: The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.Type: ApplicationFiled: May 18, 2012Publication date: October 25, 2012Inventors: Andrew Aydon Godfrey, Janelle Comita-Prevoir, Mark Cronin, Bolin Geng, Folkert Reck
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Publication number: 20120270841Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.Type: ApplicationFiled: April 15, 2012Publication date: October 25, 2012Inventors: Qi Wei, Ming Zhou, Xiaoming Xu, Charles Caldwell, Susan Harran, Lai Wang
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Publication number: 20120264750Abstract: The present invention provides: an arthropod pests control composition comprising, as active ingredients, a condensed heterocyclic compound and a diamide compound; a method for controlling arthropod pests which comprises applying effective amounts of a condensed heterocyclic compound and a diamide compound to the arthropod pests or a locus where the arthropod pests inhabit; and so on.Type: ApplicationFiled: October 18, 2010Publication date: October 18, 2012Applicant: Sumitomo Chemical Company, LimitedInventor: Junko Otsuki
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Patent number: 8288548Abstract: The present invention provides oxazolo[5,4-b]pyridin-5-yl compounds useful in the treatment of cancer.Type: GrantFiled: November 17, 2011Date of Patent: October 16, 2012Assignee: Eli Lilly and CompanyInventors: David Andrew Coates, Raymond Gilmour, Jose Alfredo Martin, Eva Maria Martin de la Nava
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Publication number: 20120258973Abstract: The invention relates to compound of the formula (I?) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: December 20, 2010Publication date: October 11, 2012Applicant: NOVARTIS AGInventors: Sangamesh Babiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Murali Chebrolu, Simona Cotesta, Samuel Hintermann, Arndt Meyer, Chetan Pandit
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Patent number: 8283360Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: December 18, 2009Date of Patent: October 9, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian
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Publication number: 20120252804Abstract: The present invention provides: an arthropod pests control composition comprising, as active ingredients, a condensed heterocyclic compound and pyriproxyfen; a method for controlling arthropod pests which comprises applying effective amounts of a condensed heterocyclic compound and pyriproxyfen to the arthropod pests or a locus where the arthropod pests inhabit; and so on.Type: ApplicationFiled: October 18, 2010Publication date: October 4, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Junko Otsuki
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Publication number: 20120252807Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.Type: ApplicationFiled: March 19, 2012Publication date: October 4, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
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Publication number: 20120252803Abstract: The present invention provides: an arthropod pests control composition comprising, as active ingredients, a condensed heterocyclic compound and a pyrethroid compound; a method for controlling arthropod pests which comprises applying effective amounts of a condensed heterocyclic compound and a pyrethroid compound to the arthropod pests or a locus where the arthropod pests inhabit; and so on.Type: ApplicationFiled: October 18, 2010Publication date: October 4, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Junko Otsuki
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Publication number: 20120245167Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: April 17, 2012Publication date: September 27, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Mitsuhiko IWAKOSHI, Ippei UEMURA
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Publication number: 20120245159Abstract: The present invention provides: an arthropod pests control composition comprising, as active ingredients, a condensed heterocyclic compound and a neonicotinoid compound; a method for controlling arthropod pests which comprises applying effective amounts of a condensed heterocyclic compound and a neonicotinoid compound to the arthropod pests or a locus where the arthropod pests inhabit; and so on.Type: ApplicationFiled: September 28, 2010Publication date: September 27, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Junko Otsuki
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Publication number: 20120238559Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: December 3, 2010Publication date: September 20, 2012Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20120238599Abstract: The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.Type: ApplicationFiled: March 19, 2012Publication date: September 20, 2012Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.Inventors: Gilnam Lee, Han Won Cho, Eun Jin Song, Hye Sun Jeon, Min Jeong Kim, Jeongbeob Seo, Albert Charles Gyorkos, Suk Young Cho
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Patent number: 8269008Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: GrantFiled: December 2, 2008Date of Patent: September 18, 2012Assignee: FibroGen, Inc.Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
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Publication number: 20120232099Abstract: The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: May 14, 2012Publication date: September 13, 2012Inventors: Richard Pracitto, John F. Kadow, John A. Bender, Brett R. Beno, Katherine A. Grant-Young, Ying Han, Piyasena Hewawasam, Andrew Nickel, Kyle E. Parcella, Kap-Sun Yeung, Louis S. Chupak
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Publication number: 20120220571Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X is O or N(R3); and R1, R2, R3 and Y are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: August 16, 2010Publication date: August 30, 2012Inventors: John S. Wai, Dai-shi Su, Catherine M. Wiscount
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Patent number: 8252793Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: GrantFiled: August 17, 2011Date of Patent: August 28, 2012Assignees: Alcon Research, Ltd., Astellas Pharma Inc.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120214824Abstract: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: December 8, 2011Publication date: August 23, 2012Inventors: Bradley Tait, Christopher Borella, Robert Chambers, Matthew Cullen
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Publication number: 20120214805Abstract: The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.Type: ApplicationFiled: October 28, 2010Publication date: August 23, 2012Inventors: Joel M. Harris, Andrew Stamford, William J. Greenlee, Santhosh Francis Neelamkavil
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120208838Abstract: A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Inventors: Amjad Ali, Christopher Franklin, Ravi Nargund, Michael Man-Chu Lo, Lin Yan, Pei Huo
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Patent number: 8242133Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: GrantFiled: April 21, 2009Date of Patent: August 14, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsuhiko Iwakoshi, Ippei Uemura
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Publication number: 20120202845Abstract: A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: September 20, 2010Publication date: August 9, 2012Inventors: Amjad Ali, Michael Man-Chu Lo, Lin Yan